Results 91 to 100 of about 1,034 (134)
Some of the next articles are maybe not open access.
Brain Research, 1986
The hypothermic effect of neurotensin (0.1 microgram) injected i.c.v. in mice is potentiated by the enkephalinase inhibitor thiorphan (10 micrograms, i.c.v.). This potentiation is not reversed by systemic naloxone. The hypothermic effect of neurotensin is not modified by the amino-peptidase inhibitor bestatin (50 micrograms, i.c.v.) nor by the ...
J Costentin, Patrick Kitabgi, I Dubuc
exaly +3 more sources
The hypothermic effect of neurotensin (0.1 microgram) injected i.c.v. in mice is potentiated by the enkephalinase inhibitor thiorphan (10 micrograms, i.c.v.). This potentiation is not reversed by systemic naloxone. The hypothermic effect of neurotensin is not modified by the amino-peptidase inhibitor bestatin (50 micrograms, i.c.v.) nor by the ...
J Costentin, Patrick Kitabgi, I Dubuc
exaly +3 more sources
Endogenous atrial natriuretic factor after endopeptidase 24.11 inhibition by Thiorphan
Peptides, 1990The neutral endopeptidase 24.11 (NEP) was shown to degrade atrial natriuretic factor (ANF) in kidney membranes. An infusion of Thiorphan (25 micrograms/min/kg x 90 min), a specific NEP inhibitor, induced an increase in plasma ANF (65 +/- 26 to 163 +/- 52 pg/ml), plasma renin activity and in norepinephrine concentrations at 50 minutes of infusion in ...
Michele Brochu +2 more
exaly +3 more sources
European Journal of Pharmacology, 1984
Thiorphan, an 'enkephalinase' inhibitor, and bestatin, an aminopeptidase inhibitor, decreased the turnover of noradrenaline and increased that of dopamine and serotonin in mouse brain regions. All effects were prevented by naloxone, indicating that when protected from the action of inactivating neuropeptidases endogenous enkephalins might affect ...
Llorens-Cortes C, J C Schwartz
exaly +3 more sources
Thiorphan, an 'enkephalinase' inhibitor, and bestatin, an aminopeptidase inhibitor, decreased the turnover of noradrenaline and increased that of dopamine and serotonin in mouse brain regions. All effects were prevented by naloxone, indicating that when protected from the action of inactivating neuropeptidases endogenous enkephalins might affect ...
Llorens-Cortes C, J C Schwartz
exaly +3 more sources
Effect of bestatin and thiorphan on [Met5]enkephalin-Arg6-Phe7-induced analgesia
European Journal of Pharmacology, 1984We investigated the effect of bestatin, a specific inhibitor of aminopeptidase and thiorphan, a specific inhibitor of enkephalinase A, on the analgesic effect induced by the intracerebral injection of heptapeptide [Met5]enkephalin-Arg6-Phe7 (MEAP) in cannulated rats.
Angelo Mario Reggiani +2 more
exaly +3 more sources
Thiorphan and acetorphan inhibit gastric secretion by a central, non-opioid mechanism in the rat
European Journal of Pharmacology, 1988Thiorphan and its prodrug, acetorphan, are two inhibitors of enkephalinase (EC 3.4.24.11), a membrane-bound peptidase which plays an important role in the metabolic degradation of enkephalins. Since exogenous opioids have been reported to both stimulate and inhibit gastric secretion, the effects of thiorphan and acetorphan were studied in conscious ...
Claude Roze, M Dubrasquet, J Chariot
exaly +3 more sources
Thiorphan and retro-thiorphan display equivalent interactions when bound to crystalline thermolysin
Biochemistry, 1989The three-dimensional structures of (S)-thiorphan and (R)-retro-thiorphan bound to thermolysin have been determined crystallographically and refined to residuals of 0.183 and 0.187 at 1.7-A resolution. Thiorphan [N-[(S)-2-(mercaptomethyl)-1-oxo-3-phenylpropyl]glycine] [HSCH2CH(CH2C6H5)CONHC-H2COOH] and retro-thiorphan [[[(R)-1-(mercaptomethyl)-2 ...
S L, Roderick +3 more
openaire +3 more sources
Thiorphan potentiation of stress-induced analgesia in the mouse
Life Sciences, 1982Experiments were done to examine the analgesic effect of thiorphan alone or in combination with stress in mice. Analgesia was assessed by measuring jump latencies from a 55 degrees C hot plate. Thiorphan exhibited weak analgesic properties evidenced by significant increases in jump latencies only after 300 mg/kg i.p. Additional experiments were done to
R, Greenberg, E H, O'Keefe
openaire +2 more sources
Bioorganic & Medicinal Chemistry Letters, 1992
Abstract Syntheses and biological activities of four thiorphan isosteres or analogs are described. The central amide linkage is replaced by ketomethylene, aminomethylene, thioamide, and trans-olefinic functionalities. Double chelation mechanism for the inhibitor-enkephalinase docking process is proposed.
Monteil Thierry +7 more
openaire +1 more source
Abstract Syntheses and biological activities of four thiorphan isosteres or analogs are described. The central amide linkage is replaced by ketomethylene, aminomethylene, thioamide, and trans-olefinic functionalities. Double chelation mechanism for the inhibitor-enkephalinase docking process is proposed.
Monteil Thierry +7 more
openaire +1 more source
Asymmetric synthesis of the enkephalinase inhibitor thiorphan
The Journal of Organic Chemistry, 1985Synthese de la N-[mercaptomethyl-2 phenyl-3 propionyl] glycine(thiorphane) a partir d'oxazolidones-2 ...
David A. Evans +2 more
openaire +1 more source
Enkephalinase ‘A’ inhibition by thiorphan: Central and peripheral cardiovascular effects
European Journal of Pharmacology, 1983On the basis of the distribution of enkephalins within the central and peripheral nervous systems as well as on responses to their administration, it has been suggested that these peptides participate in the regulation of the circulation. The present series of experiments examined the effects of thiorphan, an inhibitor of enkephalinase A, on ...
T, Baum +4 more
openaire +2 more sources